Antiasthmatic Compound 1
目录号 : GC31991AntiasthmaticCompound1是一种抗哮喘药,可用于治疗过敏性哮喘。
Cas No.:63768-49-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Antiasthmatic Compound 1 is an antiasthmatic agent, which can be used to treat allergic asthma.
[1]. Morinaka, Yasuhiro; et al. QUINOLOPYRANEE44ONEE22 CARBOXYLATE DERIVATIVES AND MEDICINE FOR ALLERGIC ASTHMA. JPS52109000A.
Cas No. | 63768-49-0 | SDF | |
Canonical SMILES | O=C(C(O1)=CC(C2=C1C3=C(NC2=O)C=CC(C)=C3)=O)O | ||
分子式 | C14H9NO5 | 分子量 | 271.22 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.687 mL | 18.4352 mL | 36.8704 mL |
5 mM | 0.7374 mL | 3.687 mL | 7.3741 mL |
10 mM | 0.3687 mL | 1.8435 mL | 3.687 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Synthesis, antiasthmatic, and insecticidal/antifungal activities of allosamidins
J Enzyme Inhib Med Chem.2019 Dec;34(1):1226-1232.PMID: 31307248DOI:10.1080/14756366.2019.1623208.
Allosamidins come from the secondary metabolites of Streptomyces species, and they have the pseudotrisaccharide structures. Allosamidins are chitinase inhibitors that can be used to study the physiological effects of chitinases in a variety of organisms. They have the novel antiasthmatic activity and insecticidal/antifungal activities. Herein, the synthesis and activities of allosamidins were summarized and analyzed.
Screening methods for antiasthmatic agents
Methods Find Exp Clin Pharmacol. 2000 Apr;22(3):191-7. PMID: 10893704DOI:
Bronchial asthma is characterized by both bronchoconstriction and airway inflammation which leads to bronchial hyperresponsiveness to various stimuli. Different mediators are implicated in asthma. As the precise etiology is not known and multiple biochemical processes are triggered by different causative factors, it is difficult to have a single drug which can effectively and simultaneously act upon different mediators. This led to an intense search for potent and safe antiasthmatic drugs. This review intends to compile different screening methods for the evaluation of new candidate drugs with potential for the treatment of asthma. These include in vitro, in vivo, receptor binding and enzymatic methods. Detailed experimental methods have been included with appropriate literature citations.
Antiasthmatic Compounds Targeting β2-Adrenergic Receptor from Perilla frutescens Improved Lung Inflammation by Inhibiting the NF-κB Signaling Pathway
J Nat Prod.2022 Nov 25;85(11):2656-2666.PMID: 36322828DOI:10.1021/acs.jnatprod.2c00767.
Asthma is a highly prevalent and heterogeneous chronic respiratory disease and is often treated with inhaled corticosteroids or in combination with a β2-adrenergic receptor (β2-AR) agonist. However, around 5% of asthma remains uncontrolled, and more effective antiasthmatic drugs with known mechanisms are in high demand. Herein, we immobilized β2-AR on the polystyrene amino microsphere surface in a one-step fashion. The successful immobilization of β2-AR was verified by scanning electron microscopy and chromatographic analysis. We screened rosmarinic acid (RA) as the bioactive compound targeting β2-AR in Perilla frutescens (L.) Britton by mass spectroscopy. The binding constant between RA and β2-AR was determined to be 2.95 × 104 M-1 by adsorption energy distribution and frontal analysis. The antiasthmatic effect and mechanism of RA were examined on a murine model of allergic asthma induced by ovalbumin (OVA) and aluminum hydroxide. The results showed that RA significantly reduced lung inflammatory cell numbers, the production of Th2 cytokines, and the secretion of total IgE, OVA-specific IgE, and eotaxin. The decreased inflammatory cell infiltration and mucus hypersecretion were associated with the inhibition of the NF-κB signaling pathway. Moreover, the mRNA expression levels of AMCase, CCL11, CCR3, Ym2, and E-selectin in the lung tissues were effectively reduced. It is the first time that RA was proven to target β2-AR and be effective in counteracting allergic airway inflammation via the NF-κB signaling pathway. Therefore, the immobilized β2-AR preserves the potential in screening antiasthmatic compounds from herbal medicine, and RA can be developed as an effective agent for the treatment of allergic asthma.
Some medicinal plants with antiasthmatic potential: a current status
Asian Pac J Trop Biomed.2011 Oct;1(5):413-8.PMID: 23569804DOI:10.1016/S2221-1691(11)60091-9.
Asthma is a common disease that is rising in prevalence worldwide with the highest prevalence in industrialized countries. Asthma affects about 300 million people worldwide and it has been estimated that a further 100 million will be affected by 2025. Since the ancient times, plants have been exemplary sources of medicine. Current asthma therapy lack satisfactory success due to adverse effect, hence patients are seeking complementary and alternative medicine to treat their asthma. Ayurveda and other Indian literature mention the use of plants in various human ailments. India has about 45,000 plant species and among them several thousand are claimed to possess medicinal properties. Researches conducted in the last few decades on the plants mentioned in ancient literature or used traditionally for asthma have shown antiasthmatic, antihistaminic and antiallergic activity. This review reveals that some plants and their extract have antiasthmatic, antihistaminic, anticholinergic and antiallergic activity.
Recent perspectives in the design of antiasthmatic agents
Pharmazie.2000 Jul;55(7):475-82.PMID: 10944772DOI:10.1002/chin.200041272.
Asthma is a common respiratory disorder. It can no longer be viewed as a reversible airway obstruction but should instead be considered primarily as an inflammatory illness that has bronchial hyperreactivity and bronchospasm as its result. There are several potential benefits as well as limitations of the currently available antiasthmatic agents such as anticholinergics, beta 2-selective agonists, methylxanthines, corticosteroids, or mast cell stabilizers. Recent trends in the design of new antiasthmatic agents include isozyme selective phosphodiesterase inhibitors, inhibitors of the biosynthesis of interleukin-4 and IL-4 antagonists, lipoxygenase and leukotriene inhibitors, thromboxane A2 receptor antagonists, potassium channel openers and monoclonal antibodies.